HRP20220936T1 - Heterocyclic amides useful as protein modulators - Google Patents

Heterocyclic amides useful as protein modulators Download PDF

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HRP20220936T1
HRP20220936T1 HRP20220936TT HRP20220936T HRP20220936T1 HR P20220936 T1 HRP20220936 T1 HR P20220936T1 HR P20220936T T HRP20220936T T HR P20220936TT HR P20220936 T HRP20220936 T HR P20220936T HR P20220936 T1 HRP20220936 T1 HR P20220936T1
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Croatia
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pyrazole
benzo
ethyl
methyl
pharmaceutically acceptable
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HRP20220936TT
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Croatian (hr)
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Adam Kenneth Charnley
Michael G. Darcy
Jason W. DODSON
Xiaoyang Dong
Terry V. Hughes
Jianxing Kang
Lara Kathryn LEISTER
Yiqian LIAN
Yue Li
John F. Mehlmann
Neysa Nevins
Joshi M. Ramanjulu
Joseph J. Romano
Gren Z. Wang
Guosen Ye
Daohua Zhang
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Glaxosmithkline Intellectual Property Development Limited
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    • A61K31/4164—1,3-Diazoles
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Claims (20)

1. Spoj koji je (E)-1-(4-(5-karbamoil-2-(1-etil-3-metil-1H-pirazol-5-karboksamido)-7-(3-morfolinopropoksi)- 1H-benzo[d]imidazol-1-il)but-2-en-1-il)-2-(1-etil-3-metil-1H-pirazol-5-karboksamido)-7-metoksi-1H-benzo[d]imidazol-5-karboksamid koji ima strukturu od [image] ili njegov tautomer, ili njegova farmaceutski prihvatljiva sol, ili njegov hidrat.1. A compound which is (E)-1-(4-(5-carbamoyl-2-(1-ethyl-3-methyl-1H-pyrazole-5-carboxamido)-7-(3-morpholinopropoxy)-1H-benzo [d]imidazol-1-yl)but-2-en-1-yl)-2-(1-ethyl-3-methyl-1H-pyrazole-5-carboxamido)-7-methoxy-1H-benzo[d] imidazole-5-carboxamide having the structure of [image] or its tautomer, or a pharmaceutically acceptable salt thereof, or its hydrate. 2. Spoj prema zahtjevu 1, koji je farmaceutski prihvatljiva sol (E)-1-(4-(5-karbamoil-2-(1-etil-3-metil-1H-pirazol-5-karboksamido)- 7-(3-morfolinopropoksi)-1H-benzo[d]imidazol-1-il)but-2-en-1-il)-2-(1-etil-3-metil-1H-pirazol-5-karboksamido) -7-metoksi-1H-benzo[d]imidazol-5-karboksamid, ili njegov tautomer.2. The compound according to claim 1, which is a pharmaceutically acceptable salt of (E)-1-(4-(5-carbamoyl-2-(1-ethyl-3-methyl-1H-pyrazole-5-carboxamido)-7-(3 -morpholinopropoxy)-1H-benzo[d]imidazol-1-yl)but-2-en-1-yl)-2-(1-ethyl-3-methyl-1H-pyrazole-5-carboxamido)-7-methoxy -1H-benzo[d]imidazole-5-carboxamide, or its tautomer. 3. Spoj prema zahtjevu 1, koji je (E)-1-(4-(5-karbamoil-2-(1-etil-3-metil-1H-pirazol-5-karboksamido)-7-(3- morfolinopropoksi)-1H-benzo[d]imidazol-1-il)but-2-en-1-il)-2-(1-etil-3-metil-1H-pirazol-5-karboksamido)-7-metoksi- 1H-benzo[d]imidazol-5-karboksamid, ili njegov tautomer.3. The compound according to claim 1, which is (E)-1-(4-(5-carbamoyl-2-(1-ethyl-3-methyl-1H-pyrazole-5-carboxamido)-7-(3-morpholinopropoxy) -1H-benzo[d]imidazol-1-yl)but-2-en-1-yl)-2-(1-ethyl-3-methyl-1H-pyrazole-5-carboxamido)-7-methoxy- 1H- benzo[d]imidazole-5-carboxamide, or a tautomer thereof. 4. Spoj prema zahtjevu 1, koji je (E)-1-((E)-4-((E)-5-karbamoil-2-((1-etil-3-metil-1H-pirazol-5) -karbonil)imino)-7-(3-morfolinopropoksi)-2,3-dihidro-1H-benzo[d]imidazol-1-il)but-2-en-1-il)-2-((1-etil -3-metil-1H-pirazol-5-karbonil)imino)-7-metoksi-2,3-dihidro-1H-benzo[d]imidazol-5-karboksamid koji ima strukturu [image] ili njegova farmaceutski prihvatljiva sol, ili njegov hidrat.4. The compound according to claim 1, which is (E)-1-((E)-4-((E)-5-carbamoyl-2-((1-ethyl-3-methyl-1H-pyrazole-5)- carbonyl)imino)-7-(3-morpholinopropoxy)-2,3-dihydro-1H-benzo[d]imidazol-1-yl)but-2-en-1-yl)-2-((1-ethyl - 3-methyl-1H-pyrazole-5-carbonyl)imino)-7-methoxy-2,3-dihydro-1H-benzo[d]imidazole-5-carboxamide having the structure [image] or a pharmaceutically acceptable salt thereof, or its hydrate. 5. Spoj prema zahtjevu 4, koji je farmaceutski prihvatljiva sol (E)-1-((E)-4-((E)-5-karbamoil-2-((1-etil-3-metil- 1H-pirazol-5-karbonil)imino)-7-(3-morfolinopropoksi)-2,3-dihidro-1H-benzo[d]imidazol-1-il)but-2-en-1-il)-2- ((1-etil-3-metil-1H-pirazol-5-karbonil)imino)-7-metoksi-2,3-dihidro-1H-benzo[d]imidazol-5-karboksamid.5. A compound according to claim 4, which is a pharmaceutically acceptable salt of (E)-1-((E)-4-((E)-5-carbamoyl-2-((1-ethyl-3-methyl-1H-pyrazole- 5-carbonyl)imino)-7-(3-morpholinopropoxy)-2,3-dihydro-1H-benzo[d]imidazol-1-yl)but-2-en-1-yl)-2- ((1- ethyl-3-methyl-1H-pyrazole-5-carbonyl)imino)-7-methoxy-2,3-dihydro-1H-benzo[d]imidazole-5-carboxamide. 6. Spoj prema zahtjevu 4, koji je (E)-1-((E)-4-((E)-5-karbamoil-2-((1-etil-3-metil-1H-pirazol-5) -karbonil)imino)-7-(3-morfolinopropoksi)-2,3-dihidro-1H-benzo[d]imidazol-1-il)but-2-en-1-il)-2-((1-etil -3-metil-1H-pirazol-5-karbonil)imino)-7-metoksi-2,3-dihidro-1H-benzo[d]imidazol-5-karboksamid.6. The compound according to claim 4, which is (E)-1-((E)-4-((E)-5-carbamoyl-2-((1-ethyl-3-methyl-1H-pyrazole-5)- carbonyl)imino)-7-(3-morpholinopropoxy)-2,3-dihydro-1H-benzo[d]imidazol-1-yl)but-2-en-1-yl)-2-((1-ethyl - 3-Methyl-1H-pyrazole-5-carbonyl)imino)-7-methoxy-2,3-dihydro-1H-benzo[d]imidazole-5-carboxamide. 7. Spoj prema zahtjevu 1, koji je (Z)-1-((E)-4-((Z)-5-karbamoil-2-((1-etil-3-metil-1H-pirazol-5) -karbonil)imino)-7-(3-morfolinopropoksi)-2,3-dihidro-1H-benzo[d]imidazol-1-il)but-2-en-1-il)-2-((1-etil -3-metil-1H-pirazol-5-karbonil)imino)-7-metoksi-2,3-dihidro-1H-benzo[d]imidazol-5-karboksamid koji ima strukturu [image] ili njegova farmaceutski prihvatljiva sol, ili njegov hidrat.7. The compound according to claim 1, which is (Z)-1-((E)-4-((Z)-5-carbamoyl-2-((1-ethyl-3-methyl-1H-pyrazole-5)- carbonyl)imino)-7-(3-morpholinopropoxy)-2,3-dihydro-1H-benzo[d]imidazol-1-yl)but-2-en-1-yl)-2-((1-ethyl - 3-methyl-1H-pyrazole-5-carbonyl)imino)-7-methoxy-2,3-dihydro-1H-benzo[d]imidazole-5-carboxamide having the structure [image] or a pharmaceutically acceptable salt thereof, or its hydrate. 8. Spoj prema zahtjevu 7, koji je farmaceutski prihvatljiva sol (Z)-1-((E)-4-((Z)-5-karbamoil-2-((1-etil-3-metil- 1H-pirazol-5-karbonil)imino)-7-(3-morfolinopropoksi)-2,3-dihidro-1H-benzo[d]imidazol-1-il)but-2-en-1-il)-2- ((1-etil-3-metil-1H-pirazol-5-karbonil)imino)-7-metoksi-2,3-dihidro-1H-benzo[d]imidazol-5-karboksamid.8. A compound according to claim 7, which is a pharmaceutically acceptable salt of (Z)-1-((E)-4-((Z)-5-carbamoyl-2-((1-ethyl-3-methyl-1H-pyrazole- 5-carbonyl)imino)-7-(3-morpholinopropoxy)-2,3-dihydro-1H-benzo[d]imidazol-1-yl)but-2-en-1-yl)-2- ((1- ethyl-3-methyl-1H-pyrazole-5-carbonyl)imino)-7-methoxy-2,3-dihydro-1H-benzo[d]imidazole-5-carboxamide. 9. Spoj prema zahtjevu 7, koji je (Z)-1-((E)-4-((Z)-5-karbamoil-2-((1-etil-3-metil-1H-pirazol-5) -karbonil)imino)-7-(3-morfolinopropoksi)-2,3-dihidro-1H-benzo[d]imidazol-1-il)but-2-en-1-il)-2-((1-etil -3-metil-1H-pirazol-5-karbonil)imino)-7-metoksi-2,3-dihidro-1H-benzo[d]imidazol-5-karboksamid.9. The compound according to claim 7, which is (Z)-1-((E)-4-((Z)-5-carbamoyl-2-((1-ethyl-3-methyl-1H-pyrazole-5)- carbonyl)imino)-7-(3-morpholinopropoxy)-2,3-dihydro-1H-benzo[d]imidazol-1-yl)but-2-en-1-yl)-2-((1-ethyl - 3-Methyl-1H-pyrazole-5-carbonyl)imino)-7-methoxy-2,3-dihydro-1H-benzo[d]imidazole-5-carboxamide. 10. Spoj prema zahtjevu 1, koji je (E)-1-(4-(5-karbamoil-2-(1-etil-3-metil-1H-pirazol-5-karboksamido)-7-(3- morfolinopropoksi)-1H-benzo[d]imidazol-1-il)but-2-en-1-il)-2-(1-etil-3-metil-1H-pirazol-5-karboksamido)-7-metoksi- 1H-benzo[d]imidazol-5-karboksamid tris hidroklorid, ili njegov tautomer.10. The compound according to claim 1, which is (E)-1-(4-(5-carbamoyl-2-(1-ethyl-3-methyl-1H-pyrazole-5-carboxamido)-7-(3-morpholinopropoxy) -1H-benzo[d]imidazol-1-yl)but-2-en-1-yl)-2-(1-ethyl-3-methyl-1H-pyrazole-5-carboxamido)-7-methoxy- 1H- benzo[d]imidazole-5-carboxamide tris hydrochloride, or a tautomer thereof. 11. Farmaceutski pripravak, naznačen time, da sadrži spoj, njegov tautomer, njegovu farmaceutski prihvatljivu sol ili njegov hidrat prema bilo kojem od zahtjeva 1-10, i farmaceutski prihvatljivu pomoćnu tvar.11. Pharmaceutical preparation, characterized in that it contains a compound, its tautomer, its pharmaceutically acceptable salt or its hydrate according to any one of claims 1-10, and a pharmaceutically acceptable excipient. 12. Spoj, njegov tautomer, njegova farmaceutski prihvatljiva sol ili njegov hidrat prema bilo kojem od zahtjeva 1-10, naznačen time, da se koristi u terapiji.12. A compound, its tautomer, its pharmaceutically acceptable salt or its hydrate according to any one of claims 1-10, indicated to be used in therapy. 13. Spoj, njegov tautomer, njegova farmaceutski prihvatljiva sol ili njegov hidrat prema bilo kojem od zahtjeva 1-10, naznačen time, da se koristi u liječenju bolesti posredovane STING-om.13. A compound, a tautomer thereof, a pharmaceutically acceptable salt thereof, or a hydrate thereof according to any one of claims 1-10, for use in the treatment of a STING-mediated disease. 14. Spoj, njegov tautomer, njegova farmaceutski prihvatljiva sol ili njegov hidrat za upotrebu kako je definirano u zahtjevu 13, gdje je bolest rak.14. A compound, a tautomer thereof, a pharmaceutically acceptable salt thereof or a hydrate thereof for use as defined in claim 13, wherein the disease is cancer. 15. Spoj, njegov tautomer, njegova farmaceutski prihvatljiva sol ili njegov hidrat za upotrebu kako je definirano u zahtjevu 13, gdje je bolest čvrsti tumor.15. A compound, a tautomer thereof, a pharmaceutically acceptable salt thereof or a hydrate thereof for use as defined in claim 13, wherein the disease is a solid tumor. 16. Spoj, njegov tautomer, njegova farmaceutski prihvatljiva sol ili njegov hidrat za upotrebu kako je definirano u zahtjevu 14, gdje je rak akutna mijeloična leukemija (AML).16. A compound, a tautomer thereof, a pharmaceutically acceptable salt thereof or a hydrate thereof for use as defined in claim 14, wherein the cancer is acute myeloid leukemia (AML). 17. Kombinacija koja sadrži spoj, njegov tautomer, njegovu farmaceutski prihvatljivu sol ili njegov hidrat prema bilo kojem od zahtjeva 1-10 i imunomodulator.17. A combination comprising a compound, a tautomer thereof, a pharmaceutically acceptable salt thereof or a hydrate thereof according to any one of claims 1-10 and an immunomodulator. 18. Kombinacija definirana u zahtjevu 17, naznačena time što je imunomodulator anti-PD-L1 agens.18. The combination defined in claim 17, characterized in that the immunomodulator is an anti-PD-L1 agent. 19. Kombinacija definirana u zahtjevu 17, naznačena time što je imunomodulator PD-1 antagonist.19. The combination defined in claim 17, characterized in that the immunomodulator is a PD-1 antagonist. 20. Kombinacija kako je definirana u zahtjevu 19, naznačena time što je PD-1 antagonist anti-PD-1 antitijelo koje je pembrolizumab.20. The combination as defined in claim 19, characterized in that the PD-1 antagonist is an anti-PD-1 antibody which is pembrolizumab.
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